BR112015022058A2 - Substituted 7-azabicycles and their use as orexin receptor modulators - Google Patents

Substituted 7-azabicycles and their use as orexin receptor modulators

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Publication number
BR112015022058A2
BR112015022058A2 BR112015022058A BR112015022058A BR112015022058A2 BR 112015022058 A2 BR112015022058 A2 BR 112015022058A2 BR 112015022058 A BR112015022058 A BR 112015022058A BR 112015022058 A BR112015022058 A BR 112015022058A BR 112015022058 A2 BR112015022058 A2 BR 112015022058A2
Authority
BR
Brazil
Prior art keywords
alkyl
compounds
pyrazolyl
pyridyl
alkoxy
Prior art date
Application number
BR112015022058A
Other languages
Portuguese (pt)
Inventor
Fitzgerald Anne
T Shireman Brock
Preville Cathy
A Dvorak Curt
R Coate Heather
P Lebold Terry
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112015022058A2 publication Critical patent/BR112015022058A2/en

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

abstract the present invention is directed to compounds of formula i: i wherein ring a is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; r1 is h, alkyl, alkoxy, hydroxyalkylene, oh, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; r2 is h, alkyl, alkoxy, hydroxyalkylene, or halo; z is nh, n-alkyl, or o; r5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. methods of making the compounds of formula i are also described. the invention also relates to pharmaceutical compositions comprising compounds of formula i. methods of using the compounds of the invention are also within the scope of the invention. tradução do resumo resumo patente de invenção "7-azabiciclos substituídos e o uso destes como moduladores do receptor de orexina" a presente invenção é direcionada aos compostos da fór-mula (i): i em que o anel a é uma fenila, naftalenila, piridila, quinolinila, isoquino-linila, imidazopiridila, furanila, tiazolila, isoxazolila, pirazolila, imidazoti-azolila, benzimidazolila ou indazolila; r1 é um radical h, alquila, alcoxila, hidroxialquileno, oh, halo, fenila, triazolila, oxazolila, isoxazolila, piridila, pirimidinila, pirazinila, piridazinila, piperazinila, pirazolila, oxadiazolila, pirrolidinila, tiofenila, morfolinila ou dialquilamino; r2 é um radical h, alquila, alcoxila, hidroxialquileno, ou halo; z é nh, n-alquila ou o; r5 é um radical piridila, pirimidinila, pirazinila, piridazinila, quinazolinila, quinoxalinila, pirazolila, benzoxazolila, imidazopirazinila, triazolopirazinila, opcionalmente substituídos por um ou dois substituintes indepen-dentemente selecionados do grupo que consiste em alquila, alcoxila ou halo; e n é 0 ou 1. os métodos de preparo dos compostos da fórmula i são também descritos. a invenção também se refere a composições farmacêuticas que compreendem compostos da fórmula i. os métodos de uso dos compostos da invenção estão também dentro do escopo da invenção.wherein the ring is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; r1 is h, alkyl, alkoxy, hydroxyalkylene, oh, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R 2 is h, alkyl, alkoxy, hydroxyalkylene, or halo; z is nh, n-alkyl, or o; r5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. methods of making the compounds of formula i are also described. the invention also relates to pharmaceutical compositions comprising compounds of formula i. methods of using the compounds of the invention are also within the scope of the invention. "substituted 7-azabicycles and their use as orexin receptor modulators" the present invention is directed to the compounds of formula (i): wherein ring a is a phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl or indazolyl; R1 is a radical h, alkyl, alkoxy, hydroxyalkylene, oh, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl or dialkylamino; R 2 is an h, alkyl, alkoxy, hydroxyalkylene, or halo radical; z is nh, n-alkyl or o; R5 is a pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl radical, optionally substituted by one or two substituents independently selected from the group consisting of alkyl, alkoxy or halo; and n is 0 or 1. The methods of preparing the compounds of formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of formula I. Methods of using the compounds of the invention are also within the scope of the invention.

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